Drug Information

Drug (ID: DG00823) and It's Reported Resistant Information

• Name: Thiethylperazine
• Synonyms: Thiethylperazine; Torecan; ETHYLTHIOPERAZINE; 1420-55-9; Tietilperazina; Thiethylperazinum; Norzine; Thiethylperazine maleate; UNII-8ETK1WAF6R; 2-(ethylthio)-10-[3-(4-methylpiperazin-1-yl)propyl]-10H-phenothiazine; 8ETK1WAF6R; 3-Ethylmercapto-10-(1'-methylpiperazinyl-4'-propyl)phenothiazine; 10H-Phenothiazine, 2-(ethylthio)-10-(3-(4-methyl-1-piperazinyl)propyl)-; 2-(ethylsulfanyl)-10-[3-(4-methylpiperazin-1-yl)propyl]-10H-phenothiazine; CHEBI:9544; 1179-69-7; 2-(Ethylthio)-10-(3-(4-methyl-1-piperazinyl)propyl)phenothiazine; 2-ethylsulfanyl-10-[3-(4-methylpiperazin-1-yl)propyl]phenothiazine; Thiethylpipezazine; GS-95; Theithylperazine; 2-(Ethylthio)-10-[3-(4-methyl-1-piperazinyl)propyl]phenothiazine; Tietilperazina [DCIT]; Phenothiazine, 2-(ethylthio)-10-(3-(4-methyl-1-piperazinyl)propyl)-; 10H-Phenothiazine, 2-(ethylthio)-10-[3-(4-methyl-1-piperazinyl)propyl]-; Thiethylperazinum [INN-Latin]; 2-Ethylthio-10-(3-(4-methylpiperazin-1-yl)propyl)phenothiazine; Thioethylperazine; MLS002154140; Phenothiazine, 2-(ethylthio)-10-[3-(4-methyl-1-piperazinyl)propyl]-; Thiethylperazine [USAN:INN:BAN]; 2-(ethylthio)-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine; NSC130044; HSDB 3400; Norzine (*Dimaleate*); SMR001233447; EINECS 215-819-0; GS-95 (*Dimaleate*); Thiethylperazine (USAN/INN); Norzine (Salt/Mix); Torecan (Salt/Mix); Tresten (Salt/Mix); CHEMBL1378; SCHEMBL49124; GTPL7306; DTXSID1023651; BDBM78436; cid_3085006; BCP09601; Thiethylperazine maleate (Salt/Mix); ZINC22446674; DB00372; NCGC00262537-04; AB00514742; C07132; D02354; L000871; Q372725; 2-(Ethylthio)-10-[3-(4-methyl-1-piperazinyl)propyl]phenthiazine; 2-(ethylthio)-10-[3-(4-methylpiperazino)propyl]phenothiazine;malic acid; 2-(Ethylsulfanyl)-10-[3-(4-methyl-1-piperazinyl)propyl]-10H-phenothiazine #; 2-(ethylthio)-10-[3-(4-methyl-1-piperazinyl)propyl]phenothiazine;2-hydroxybutanedioic acid; 2-ethylsulfanyl-10-[3-(4-methylpiperazin-1-yl)propyl]phenothiazine;2-oxidanylbutanedioic acid
• Indication:
  In total 1 Indication(s)
  Nausea [ICD-11: MD90]; Approved; [1]
• Target: Dopamine D2 receptor (D2R); DRD2_HUMAN; [1]
• Formula: C22H29N3S2
• IsoSMILES: CCSC1=CC2=C(C=C1)SC3=CC=CC=C3N2CCCN4CCN(CC4)C
• InChI: 1S/C22H29N3S2/c1-3-26-18-9-10-22-20(17-18)25(19-7-4-5-8-21(19)27-22)12-6-11-24-15-13-23(2)14-16-24/h4-5,7-10,17H,3,6,11-16H2,1-2H3
• InChIKey: XCTYLCDETUVOIP-UHFFFAOYSA-N
• PubChem CID: 5440
• ChEBI ID: CHEBI:9544
• TTD Drug ID: D0Y0ER
• DrugBank ID: DB00372

Type(s) of Resistant Mechanism of This Drug

  DISM: Drug Inactivation by Structure Modification

  UAPP: Unusual Activation of Pro-survival Pathway

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-01: Infectious/parasitic diseases

Bacterial infection [ICD-11: 1A00-1C4Z]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Drug Inactivation by Structure Modification (DISM)

Key Molecule: Vancomycin/teicoplanin A-type resistance protein VanA (VANA) [1]

• Molecule Alteration: Expression; Inherence
• Sensitive Disease: Lactobacillus casei infection [ICD-11: 1A00-1C4Z]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: Enterococcus faecium strain; 1352
• In Vitro Model: Streptococcus faecium strain; 1352
• Experiment for Drug Resistance: agar dilution method
• Mechanism Description: Resistance to vancomycin in enterococci is mainly caused by expression of enzymes such as ligase, dehydrogenase, carboxypeptidase and carboxypeptidase which are encoded by genes such as vanA and vanB. Phenothiazines such as chlorpromazine are well known to deactivate a large number of enzymes. The reversal of vancomycin resistance may be due to enzyme inactivation.

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: D-alanine--D-alanine ligase (Q5MPQ2) [1]

• Molecule Alteration: Expression; Inherence
• Sensitive Disease: Lactobacillus casei infection [ICD-11: 1A00-1C4Z]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: Enterococcus faecium strain; 1352
• In Vitro Model: Streptococcus faecium strain; 1352
• Experiment for Drug Resistance: agar dilution method
• Mechanism Description: Resistance to vancomycin in enterococci is mainly caused by expression of enzymes such as ligase, dehydrogenase, carboxypeptidase and carboxypeptidase which are encoded by genes such as vanA and vanB. Phenothiazines such as chlorpromazine are well known to deactivate a large number of enzymes. The reversal of vancomycin resistance may be due to enzyme inactivation.

References

• Ref 1: Enhancement of vancomycin activity by phenothiazines against vancomycin-resistant Enterococcus faecium in vitro .Basic Clin Pharmacol Toxicol. 2010 Aug;107(2):676-9. doi: 10.1111/j.1742-7843.2010.00558.x. Epub 2010 Mar 28. 10.1111/j.1742-7843.2010.00558.x